Synthesis of a Tyr-Tyr dipeptide library and evaluation against tumor cells

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dc.contributorLaboratório de Biologia Molecularpt_BR
dc.contributorLaboratório de Genéticapt_BR
dc.contributor.authorVasconcelos, Stanley N. S.pt_BR
dc.contributor.authorSciani, Juliana Mozerpt_BR
dc.contributor.authorMambelli, Nicole Carolinept_BR
dc.contributor.authorStefani, Hélio A.pt_BR
dc.date.accessioned2020-07-09T21:21:14Z-
dc.date.available2020-07-09T21:21:14Z-
dc.date.issued2018-
dc.identifier.citationVasconcelos SN.S., Sciani JM, Mambelli NC, Stefani HA.. Synthesis of a Tyr-Tyr dipeptide library and evaluation against tumor cells. Med. Chem.. 2018;14(7):709-14. doi:10.2174/1573406414666180309153142.pt_BR
dc.identifier.issn1573-4064-
dc.identifier.urihttps://repositorio.butantan.gov.br/handle/butantan/2554-
dc.description.abstractBACKGROUND:Structural component of proteins and peptides, amino acids have been used as building blocks in the synthesis of more complex molecules with antitumor activity against several types of cancer. OBJECTIVE:The search for new anticancer compounds is ongoing, especially for cancers that are very aggressive and have poor prognoses, such as leukemia. METHOD:Here, we report a method to synthesize Tyr-Tyr dipeptides via sonochemistry reactions followed by functionalization of these Tyr-Tyr dipeptides with Suzuki-Miyaura and Sonogashira crosscoupling reactions in good yields. Twelve different Tyr-Tyr dipeptides were investigated against three cell lines: HaCaT; Jurkat-E6; and A2058. RESULTS:Some of the Tyr-Tyr dipeptides showed activity against Jurkat-E6 leukaemia cells at low concentration, decreasing their viability, but not against non-tumor HaCaT cells, suggesting a cytotoxicity specific to tumor cells. CONCLUSION:All dipeptides were able to decrease the viability of Jurkat cell line, however the A2058 cell line did not respond well to treatment with the peptides. Some of the modified Tyr-Tyr dipeptides presented selective activity on leukemic tumor cells.pt_BR
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)pt_BR
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)pt_BR
dc.format.extentp. 709-714pt_BR
dc.languageengpt_BR
dc.publisherBentham Science Publ LTDpt_BR
dc.relation.ispartofMedicinal Chemistrypt_BR
dc.titleSynthesis of a Tyr-Tyr dipeptide library and evaluation against tumor cellspt_BR
dc.typeArticlept_BR
dc.identifier.doi10.2174/1573406414666180309153142pt_BR
dc.identifier.urlhttp://dx.doi.org/10.2174/1573406414666180309153142pt_BR
dc.contributor.externalUniversidade de São Paulo (USP)¦¦Brasilpt_BR
dc.publisher.cityAmsterdampt_BR
dc.identifier.citationvolume14pt_BR
dc.identifier.citationissue7pt_BR
dc.subject.keywordTyrosinept_BR
dc.subject.keywordPeptidespt_BR
dc.subject.keywordCross-couplingpt_BR
dc.subject.keywordTriazolept_BR
dc.subject.keywordTumor cellspt_BR
dc.relation.ispartofabbreviatedMed. Chem.pt_BR
dc.identifier.citationabntv. 14, n. 7, p. 709-714, 2018pt_BR
dc.identifier.citationvancouver2018;14(7):709-14pt_BR
dc.publisher.countryNetherlandspt_BR
dc.contributor.butantanMambelli, Nicole Caroline|:Aluno|:Laboratório de Genética|:pt_BR
dc.contributor.butantanSciani, Juliana Mozer|:Técnico:Docente Colaborador PPGTOX|:Laboratório de Biologia Molecular|:pt_BR
dc.sponsorship.butantanConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)¦¦308.320/2010-7pt_BR
dc.sponsorship.butantanFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)¦¦2013/17960-7pt_BR
dc.identifier.bvsccBR78.1pt_BR
dc.identifier.bvsdbIBProdpt_BR
item.fulltextCom Texto completo-
item.grantfulltextembargo_29990101-
item.openairetypeArticle-
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